GW806742X


Catalog No. size PriceQuantity
M6623-2 2mg solid $110
M6623-10 10mg solid $436

Description

Cas:579515-63-2

Product Information:

GW806742X is a Mixed Lineage Kinase Domain-Like protein (MLKL) inhibitor which binds the MLKL pseudokinase domain with a Kd value of 9.3 μM and has anti-necroptosis activity. GW806742X has activity against VEGFR2.

 

IC50 & Target: Kd: 9.3 μM (MLKL)[1]

 

Molecular Weight: 573.55

 

Formula: C₂₅H₂₂F₃N₇O₄S

 

Smiles Code:

O=S(C1=CC=CC(NC2=NC=CC(N(C)C3=CC=C(NC(NC4=CC=C(OC(F)(F)F)C=C4)=O)C=C3)=N2)=C1)(N)=O

 

Shipping:

Room temperature in continental US; may vary elsewhere.

 

Storage:

4°C, sealed storage, away from moisture

 

In Vitro:

GW806742X (0.1-10000 nM) rescues 50% of wild-type mouse dermal fibroblasts (MDFs) from TSQ-induced necroptosis with an IC50< 50 nM when 1 ng/mL TNF is used.

GW806742X (1 μM) retards MLKL translocation to the membrane.

 

 

References

 

  1. Hildebrand JM, et al. Activation of the pseudokinase MLKL unleashes the four-helix bundle domain to induce membrane localization and necroptotic cell death. Proc Natl Acad Sci U S A. 2014 Oct 21;111(42):15072-7.

 

  1. Yan B, et al. Discovery of a new class of highly potent necroptosis inhibitors targeting the mixed lineagekinase domain-like protein. Chem Commun (Camb). 2017 Mar 28;53(26):3637-3640.

 

Products are for research use only. Not for human use.

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